Merck Sharp + Dohme Corp.

Schering Corporation

David James Cole

Duane A Burnett

Hubert B Josien

Wen-Lian Wu

Dmitri A Pissarnitski

Hongmei Li

Zhiqiang Zhao

Ruo Xu

Chad E Bennett

Martin Domalski

John W Clader

Jing Su

Theodros Asberom

Haiqun Tang

Thavalakulamgara K Sasikumar

Thomas A Bara

Chad E Knutson

Li Qiang

Mark D McBriar

Murali Rajagopalan

William J Greenlee

Zhaoning Zhu

Anandan Palani

Xianhai Huang

Malcolm Maccoss

Zhong-Yue Sun

Xiaoxiang Liu

Jun Qin

Troy McCracken

Mary Ann Caplen

Pawan Dhondi

Monica L Vicarel

Mary Anne Caplen

Thavalakulamgar Sasikumar

Martin S Domalski

Thomas Bara

Thavalakulamgar K Sasikumar

In its many embodiments, the present invention provides a novel class of heterocyclic compounds of the formula: as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more disease associated with the central nervous system using such compounds or pharmaceutical compostions. 

Gamma secretase modulators

The present invention is directed to novel tricyclic heterocycles of structural formula I which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved. 

Tricyclic heterocycles useful as dipeptidyl peptidase-IV inhibitors

This invention discloses novel gamma secretase inhibitors of the formula: Rand R, or Rand R, or Rand R, together with the atoms to which they are bound, can form a fused cycloalkyl or fused heterocycloalkyl ring. The cycloalkyl ring or the heterocycloalkyl ring can be optionally substituted with one or more substituents. One or more compounds of formula (I), or formulations comprising such compounds, may be useful, e.g. in treating Alzheimer's Disease.

Benzenesulfonyl-chromane, thiochromane, tetrahydronaphthalene and related gamma secretase inhibitors

This invention discloses novel gamma secretase inhibitors of the formula: Rand R, or Rand R, or Rand R, together with the atoms to which they are bound, can form a fused cycloalkyl or fused heterocycloalkyl ring. The cycloalkyl ring or the heterocycloalkyl ring can be optionally substituted with one or more substitutents. One or more compounds of formula (I), or formulations comprising such compounds, may be useful, e.g. in treating Alzheimer's Disease.

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Springfield, NJ, United States of America

David James Cole